1. PROTAC
  2. Molecular Glues
  3. VAV1 degrader-3

VAV1 degrader-3 (Example 185) 是一种具有口服活性的 VAV1 分子胶 降解剂 (DC50: 7 nM)。VAV1 degrader-3 可降低免疫细胞活化、免疫细胞增殖和各种细胞因子的产生。VAV1 degrader-3 可用于研究炎症或自身免疫性疾病。VAV1 degrader-3 可抑制实验性自身免疫性脑脊髓炎 (EAE) 小鼠模型、胶原诱导性关节炎 (CIA) 小鼠模型等模型的疾病进展。

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VAV1 degrader-3 Chemical Structure

VAV1 degrader-3 Chemical Structure

CAS No. : 3050683-38-7

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

VAV1 degrader-3 (Example 185) is an orally active VAV1 molecular glue degrader (DC50: 7 nM). VAV1 degrader-3 reduces immune cell activation, immune cell proliferation and the production of various cytokines. VAV1 degrader-3 can be used for research of inflammatory or autoimmune disorder. VAV1 degrader-3 inhibits disease progression in experimntal autoimmune encephalomyelitis (EAE) mouse model, Collagen-induced arthritis (CIA) mouse model, etc.[1].

体外研究
(In Vitro)

VAV1 degrader-3 (0-1 μM, 24 h) 抑制 B 细胞受体介导的活性,具体而言,VAV1 degrader-3 抑制从人血白细胞分离的 PBMC 细胞中的 CD69 表达和 IL-6、lgG 分泌[1]
VAV1 degrader-3 (0-1 μM, 24 h) 抑制原代 T 细胞中 T 细胞受体介导的 CD69 活化、IL-2 分泌和增殖[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

VAV1 degrader-3 (1-15 mg/kg,口服) 可抑制 MOGss-ss 诱发的多发性硬化症实验性自身免疫性脑脊髓炎 (EAE) 小鼠模型中的疾病进展[1]
VAV1 degrader-3 (1 mg/kg,口服) 可抑制 T 细胞转移诱发的结肠炎模型中的疾病进展,并降低结肠组织中钙卫蛋白亚基 (S100a8/S100a9) 的表达[1]
VAV1 degrader-3 (1 mg/kg,口服) 还可抑制胶原诱发性关节炎 (CIA) 小鼠模型中的疾病进展[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

392.83

Formula

C22H17ClN2O3

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

VAV1 degrader-3 相关分类

  • 摩尔计算器

  • 稀释计算器

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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VAV1 degrader-3
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